Determination of nuvenzepine in human plasma by a sensitive sup 3 Hpirenzepine radioreceptor binding assay

Journal Article · Fri Feb 01 00:00:00 EST 1991 · Journal of Pharmaceutical Sciences; (United States)

DOI:https://doi.org/10.1002/jps.2600800219· OSTI ID:5557039

Caselli, G; Ferrari, M P; Tonon, G; Clavenna, G; Borsa, M ^[1]

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1. Research Development Laboratories, Dompe Farmaceutici S.p.A., Milano (Italy)

A sensitive method for the quantitation of small amounts of nuvenzepine, a new M1-selective antimuscarinic drug, in plasma is described. The analytical method involves the use of a radioreceptor binding assay based on {sup 3}Hpirenzepine displacement in rat cerebral cortex homogenates; no previous extraction is required. The method is reliable, with an interassay CV ranging from 5 to 10%, and allows the analysis of greater than 100 samples/experiment. The limit of detection is {approximately} 0.1 ng/assay. Using this method we have determined the plasma levels of nuvenzepine in eight healthy volunteers treated PO with 15 or 25 mg of nuvenzepine.HCl. The pharmacokinetic parameters obtained were (for 15 and 25 mg): Cmax, 64 and 131 ng/mL; AUC0-infinity, 851 and 1379 ng.h/mL; t1/2, 8.6 and 7.2 h. These values are in good agreement with those obtained using an HPLC method. Therefore, this radioreceptor binding assay proved to be simple, rapid, and specific for the determination of low levels of nuvenzepine in human plasma.

• OSTI ID: 5557039
• Journal Information: Journal of Pharmaceutical Sciences; (United States), Vol. 80:2; ISSN 0022-3549
• Country of Publication: United States
• Language: English

Related Subjects

59 BASIC BIOLOGICAL SCIENCES
PARASYMPATHOLYTICS
RADIORECEPTOR ASSAY
BLOOD PLASMA
DOSE-RESPONSE RELATIONSHIPS
MAN
ORAL ADMINISTRATION
TRITIUM COMPOUNDS
ANIMALS
AUTONOMIC NERVOUS SYSTEM AGENTS
BIOLOGICAL MATERIALS
BLOOD
BODY FLUIDS
DRUGS
HYDROGEN COMPOUNDS
ISOTOPE APPLICATIONS
MAMMALS
MATERIALS
PRIMATES
TRACER TECHNIQUES
VERTEBRATES
550201* - Biochemistry- Tracer Techniques